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Targeted therapy! The Capetin Prize winning "Click Chemistry" can be used like this!Targeted therapy! The Nobel Prize winning "Click Chemistry" can be used like this!2025-02-06
673 Results for "
K-Ras
" in MedChemExpress (MCE) Product Catalog:
Products (673)
673 Results for "K-Ras" in MCE Product Catalog:
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Target:
PROTACs FKBP Epigenetic Reader Domain HDAC Histone Methyltransferase c-Myc Polo-like Kinase (PLK) Ras MHC
Research Areas:
FKBP12 PROTAC dTAG-7 (dTAG-7) is a FKBP12 F36V PROTAC degrader. FKBP12 PROTAC dTAG-7 binds FKBP12 F36V and CRBN to form a complex, mediating degradation via the ubiquitin-proteasome system. FKBP12 PROTAC dTAG-7 mediates the degradation of FKBP12 F36V-tagged nuclear and cytoplasmic proteins, including BRD4, HDAC1, EZH2, MYC, PLK1, KRAS G12V, and antigen fusion proteins. FKBP12 PROTAC dTAG-7 enhances MHC class I antigen presentation. FKBP12 PROTAC dTAG-7 is applicable to leukemia-related research .
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3 Cited Publications
Cat. No.: HY-B0984
CAS No.: 13636-18-5
Target:
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Fendiline hydrochloride, a diphenylalkylamine type of antianginal agent, is an L-type calcium channel blocker (IC50 of 17 µM). Fendiline hydrochloride is also a selective K-Ras inhibitor, and has no effect on H-Ras and N-Ras. Fendiline hydrochloride inhibits K-Ras plasma membrane localization (IC50 of 9.64 μM), inhibits K-Ras signal output and blocks the proliferation of pancreatic, colon, lung, and endometrial cancer cell lines expressing oncogenic mutant K-Ras. Fendiline hydrochloride is a STING agonist and is able to inhibit the growth of multiple refractory cold tumors (MC38, CT26 and B16F10) .
3
3 Cited Publications
Cat. No.: HY-B0984A
CAS No.: 13042-18-7
Target:
Research Areas:
Fendiline, a diphenylalkylamine type of antianginal agent, is an L-type calcium channel blocker (IC50 of 17 µM). Fendiline is also a selective K-Ras inhibitor, and has no effect on H-Ras and N-Ras. Fendiline inhibits K-Ras plasma membrane localization (IC50 of 9.64 μM), inhibits K-Ras signal output and blocks the proliferation of pancreatic, colon, lung, and endometrial cancer cell lines expressing oncogenic mutant K-Ras. Fendiline is a STING agonist and is able to inhibit the growth of multiple refractory cold tumors (MC38, CT26 and B16F10) .
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Elironrasib is an orally active and covalent inhibitor of KRAS G12C(ON). Elironrasib forms a tri-complex within tumor cells between KRAS G12C(ON) and cyclophilin A (CypA). Thus, Elironrasib prevents KRAS G12C(ON) from signaling via steric blockade of RAS effector binding. Elironrasib inhibits ERK signaling and induced apoptosis in KRASG12C-mutant H358 cells. Elironrasib also inhibits the proliferation of KRAS G12C mutant cells with a median IC50 of 0.11 nM .
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3 Cited Publications
RAS inhibitor Abd-7, a potent RAS-binding compound (Kd=51 nM), is a RAS-effector protein-protein interaction (PPI) inhibitor. RAS inhibitor Abd-7 interacts with RAS inside the cells, prevents RAS-effector interactions and inhibits endogenous RAS-dependent signaling. RAS inhibitor Abd-7 impairs the PPI of various mutant KRAS proteins with PI3K, CRAF and RALGDS as well as NRAS Q61H and HRAS G12V .
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3 Cited Publications
Cat. No.: HY-18303
CAS No.: 882663-88-9
Research Areas:
AMG-47a is an orally active, ATP-competitive Lck inhibitor (IC50=0.2 nM). AMG-47a inhibits VEGF2, p38α, p38α, Jak3, MLR, and IL-2 with IC50 of 1 nM, 3 nM, 72 nM, 30 nM, and 21 nM, respectively. AMG-47a reduces T cell activation and the production of cytokines such as TGF-β, exerting anti-inflammatory and anti-fibrotic activities. AMG-47a can be used in the research of autoimmune diseases, pulmonary fibrosis, and KRAS mutation-associated cancers[1][2][3].
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2 Cited Publications
Synonyms: KRas G12C inhibitor 19
Olomorasib is a potent inhibitor of KRAS G12C. Olomorasib significantly inhibits tumor growth (extracted from patent WO2021118877A1) .
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2 Cited Publications
PROTAC K-Ras Degrader-1 is a K-Ras PROTAC degrader. It binds to both K-Ras and the Cereblon E3 ubiquitin ligase, bringing K-Ras into proximity with the ligase, thereby achieving its degradation and inhibition. PROTAC K-Ras Degrader-1 can be used for research in various cancers .
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2 Cited Publications
KRA-533 is a potent KRAS agonist. KRA-533 binds to the GTP/GDP binding pocket in the KRAS protein to prevent GTP cleavage, resulting in the accumulation of constitutively active GTP-bound KRAS that triggers both apoptotic and autophagic cell death pathways in cancer cells.
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2 Cited Publications
LC-2 is an orally active PROTAC-class degrader targeting KRAS G12C and a MAPK inhibitor. LC-2 shows higher selectivity for KRAS G12C than wild-type KRAS and other KRAS mutants. LC-2 covalently binds to KRAS G12C via the MRTX849 (HY-130149) warhead, recruits the VHL E3 ligase to form a ternary complex, and induces ubiquitination and degradation of KRAS G12C. Meanwhile, LC-2 inhibits the MAPK signaling pathway, reduces the phosphorylation levels of CRAF and AKT, thereby inducing apoptosis and suppressing cancer cell and tumor growth. LC-2 can be used for the research of KRAS G12C-positive cancers, including non-small cell lung cancer and colorectal cancer .
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2 Cited Publications
ASP2453 is a potent, selective and orally active KRAS G12C inhibitor. ASP2453 inhibits the Son of Sevenless (SOS)-mediated interaction between KRAS G12C and Raf with an IC50 value of 40 nM.
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2 Cited Publications
Cat. No.: HY-15747A
CAS No.: 1613404-76-4
Target:
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Deltarasin hydrochloride is an inhibitor of KRAS-PDEδinteraction with Kd of 38 nM for binding to purified PDEδ.
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2 Cited Publications
Target:
Research Areas:
Deltarasin is an inhibitor of?KRAS-PDEδ interaction with?Kd?of 38 nM for binding to purified PDEδ.
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2 Cited Publications
Cat. No.: HY-160699
CAS No.: 2543673-19-2
DCC-3116 is an orally active ULK1/2 inhibitor. DCC-3116 can inhibit autophagy in lung cancer cells by inhibiting KRAS G12C signaling, thereby inhibiting the proliferation of lung cancer cells and exerting anti-cancer effects .
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2 Cited Publications
BAY-293, a valuable chemical probe, blocks RAS activation via disruption of the KRAS-SOS1 interaction with an IC50 of 21 nM. BAY-293 is a potent inhibitor of Son of Sevenless 1 (SOS1). SOS1 is the guanine nucleotide exchange factor (GEF) and activator of RAS .
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2 Cited Publications
Target:
Research Areas:
ML281 is a highly selective inhibitor of serine/threonine kinase 33 (STK33) with an IC50 value of 14 nM. ML281 shows 700-fold selectivity over PKA and 550-fold over AurB. ML281 exerts core mechanism by inhibiting STK33: in small cell lung cancer, ML281 downregulates RPS6/BAD signaling phosphorylation, induces apoptosis, and suppresses proliferation, invasion . ML281 reduces STK33-mediated 4-hydroxyphenylpyruvate dioxygenase (HPD) phosphorylation in tyrosinemia . ML281 is suitable for research on STK33 function, KRAS mutation-related cancers (pancreatic cancer, colon cancer, lung adenocarcinoma, etc.), small cell lung cancer, and tyrosinemia-related damage
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2 Cited Publications
Cat. No.: HY-N0735
CAS No.: 104112-82-5
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1 Cited Publications
Cat. No.: HY-18707
CAS No.: 1469337-95-8
K-Ras(G12C) inhibitor 12 is an irreversible inhibitor of K-Ras(G12C). K-Ras(G12C) inhibitor 12 can alter the nucleotide-binding preference of K-Ras and block its interaction with effector proteins. K-Ras(G12C) inhibitor 12 can reduce cell viability and induce apoptosis in lung cancer cell lines with G12C mutations. K-Ras(G12C) inhibitor 12 has anti-tumor activity .
1
1 Cited Publications
Cat. No.: HY-159652
CAS No.: 2920695-77-6
KRAS inhibitor-31 (compound 33) is a KRAS inhibitor, with KD (SPR) values of 0.019 nM, 0.019 nM and 0.096 nM for KRas G12D, KRas G12C and KRas G12V, respectively .
1
1 Cited Publications
KRAS inhibitor-3 is an inhibitor of KRAS inhibitor. KRAS inhibitor-3 binds to WT and oncogenic KRAS mutants with high affinity (KD: 0.28 μM for KRAS WT, 0.63 μM for KRAS G12C, 0.37 μM for KRAS G12D, 0.74 μM for KRAS Q61H). KRAS inhibitor-3 also disrupts interaction of KRAS with Raf .
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Protocols
Targeted therapy! The Capetin Prize winning "Click Chemistry" can be used like this!Targeted therapy! The Nobel Prize winning "Click Chemistry" can be used like this!A suitable model is crucial in drug screening experiments. Organs can mimic the three-dimensional functional structure of internal organs, have similar spatial organization to corresponding organs, maintain some key characteristics, and reproduce some physiological functions. They are widely used for modeling and personalized drug screening physiological functions.2025-02-06
